Asymmetric Synthesis of Imidazo[2,1‐a]isoquinolin‐3‐ones with Dihydroisoquinolines and N‐substituted Amino Acids

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AbstractA mild direct synthesis of chiral imidazo[2,1‐a]isoquinolin‐3‐one derivatives with dihydroisoquinolines and N‐substituted amino acids have been developed. By the use of easily accessible DCC as condensation reagent at ambient temperature, a series of imidazo[2,1‐a]isoquinolin‐3‐ones can be assembled readily in low to good yields with low to excellent dr values. Interestingly, the use of N‐substituted L‐Threonine and L‐Serine afforded oxazino[2,3‐a]isoquinolin‐4‐one derivatives with good diastereoselectivities.